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PF-04802367 - 98%, high purity , CAS No.1962178-27-3

COA

Grade & Purity:

≥98%

Cas Number: 1962178-27-3
Molecular Weight: 361.78

In stock

Item Number

P646646

Grouped product items
SKU	Size	Availability	Price
P646646-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$260.90
P646646-10mg	10mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$420.90
P646646-25mg	25mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$840.90
P646646-50mg	50mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$1,340.90

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Basic Description

Specifications & Purity	≥98%
Biochemical and Physiological Mechanisms	PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC 50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay.xa0PF-04802367 shows desirable central nervous system (CNS)xa0properties and potency. PF-
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available.
Product Description	PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC 50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. PF-04802367 shows desirable central nervous system (CNS) properties and potency. PF-04802367 is equally effective at inhibition of the two known GSK-3 isoforms ( GSK-3α and GSK-3β ) with IC 50 values of 10.0 and 9.0 nM in mobility shift assays, respectively In Vitro PF-04802367 (PF-367) is efficient at inhibiting GSK-3β enzymatic activity in vitro with ligand and lipophilic efficiency scores of 0.46 and 7.0, respectively. PF-367 has reasonable in vitro stability in human hepatic microsomes (t 1/2 =78.7 min), has excellent passive permeability. In a stable inducible CHO cell line over-expressing GSK-3β and its substrate tau, PF-367 inhibited phosphorylation of tau with an IC 50 of 466 nM. PF-367 has good cell viability (IC 50 of 117 μM in THLE cytotoxicity assays) and an IC 50 >100 μM in a hERG screening assay. PF-367 shows significant right shifts against β-catenin translocation in HeLa cells with EC 50 of 6.2 μM, gene transcription in U20S cells with EC 50 of 20.6 μM, and cell proliferation in HeLa cells as evaluated by Ki-67 incorporation with EC 50 of 9.0 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo PF-04802367 (PF-367) a potent GSK-3 inhibitor with exceptional kinome selectivity that modulates phosphorylated tau levels in vivo. Inhibition of phosphorylation of tau in brain by PF-367 (A single subcutaneous of 1, 3.2, 10, 32 or 50 mg/kg) is dose-dependent . PF-04802367 (PF-367), a potent type-I dual GSK-3α/β inhibitor, showing promising absorption; distribution, metabolism and elimination (ADME) properties combined with robust CNS/peripheral p-Tau and muscle phosphorylated glycogen synthase (pGS) inhibition in vivo. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Sprague-Dawley rats Dosage: 1, 3.2, 10, 32 or 50 mg/kg Administration: A single subcutaneous Result: Inhibition of phosphorylation of tau in brain is dose-dependent. Form:Solid IC50& Target:GSK-3α 10 nM (IC 50 ) GSK-3β 9 nM (IC 50 )

Names and Identifiers

Smiles	O=C(C1=C(C2=CC=C(OC)C(Cl)=C2)OC=N1)NCCCN3N=CN=C3
Molecular Weight	361.78

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